Clinical data | |
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Trade names | Lullan |
AHFS/ Drugs.com | International Drug Names |
Routes of administration | Oral |
ATC code |
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Legal status | |
Legal status |
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Pharmacokinetic data | |
Protein binding | 92% [1] |
Metabolism | Hepatic [1] |
Elimination half-life | 1.9–2.5 hours [1] [2] |
Excretion | Renal (0.4% as unchanged drug) [1] |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C23H30N4O2S |
Molar mass | 426.58 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. [1] It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania. [3] [4]
Its primary uses are in the treatment of schizophrenia and bipolar mania. [3] [4]
In a clinical trial that compared it to haloperidol in the treatment of schizophrenia it was found to produce significantly superior overall symptom control. [5] In another clinical trial perospirone was compared with mosapramine and produced a similar reduction in total PANSS score, except with respect to the blunted affect part of the PANSS negative score, in which perospirone produced a significantly greater improvement. [6] In an open-label clinical trial comparing aripiprazole with perospirone there was no significant difference between the two treatments discovered in terms of both efficacy and tolerability. [7] In 2009 a clinical trial found that perospirone produced a similar reduction of PANSS score than risperidone and the extrapyramidal side effects was similar in both frequency and severity between groups. [8]
A meta-analysis published in 2013 found that it is statistically significantly less efficacious than other second-generation antipsychotics. [9]
Has a higher incidence of extrapyramidal side effects than the other atypical antipsychotics, but still less than that seen with typical antipsychotics. [1] [10] A trend was observed in a clinical trial comparing mosapramine with perospirone that favoured perospirone for producing less prominent extrapyramidal side effects than mosapramine although statistical significant was not reached. [6] It may produce less QT interval prolongation than zotepine, as in one patient who had previously been on zotepine switching to perospirone corrected their prolonged QT interval. [11] It also tended to produce less severe extrapyramidal side effects than haloperidol in a clinical trial comparing the two (although statistical significance was not reached). [5]
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse. [12] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite. [13] Other symptoms may include restlessness, increased sweating, and trouble sleeping. [13] Less commonly there may be a felling of the world spinning, numbness, or muscle pains. [13] Symptoms generally resolve after a short period of time. [13]
There is tentative evidence that discontinuation of antipsychotics can result in psychosis. [14] It may also result in reoccurrence of the condition that is being treated. [15] Rarely tardive dyskinesia can occur when the medication is stopped. [13]
Perospirone binds to the following receptors with very high affinity (as an antagonist unless otherwise specified): [9] [16] [17] [18] [19] [20]
And the following receptor with high affinity: [9]
And the following with moderate affinity: [9]
And with low affinity for the following receptor: [9]
Withdrawal of antipsychotic drugs after long-term therapy should always be gradual and closely monitored to avoid the risk of acute withdrawal syndromes or rapid relapse.
Clinical data | |
---|---|
Trade names | Lullan |
AHFS/ Drugs.com | International Drug Names |
Routes of administration | Oral |
ATC code |
|
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Protein binding | 92% [1] |
Metabolism | Hepatic [1] |
Elimination half-life | 1.9–2.5 hours [1] [2] |
Excretion | Renal (0.4% as unchanged drug) [1] |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C23H30N4O2S |
Molar mass | 426.58 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. [1] It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania. [3] [4]
Its primary uses are in the treatment of schizophrenia and bipolar mania. [3] [4]
In a clinical trial that compared it to haloperidol in the treatment of schizophrenia it was found to produce significantly superior overall symptom control. [5] In another clinical trial perospirone was compared with mosapramine and produced a similar reduction in total PANSS score, except with respect to the blunted affect part of the PANSS negative score, in which perospirone produced a significantly greater improvement. [6] In an open-label clinical trial comparing aripiprazole with perospirone there was no significant difference between the two treatments discovered in terms of both efficacy and tolerability. [7] In 2009 a clinical trial found that perospirone produced a similar reduction of PANSS score than risperidone and the extrapyramidal side effects was similar in both frequency and severity between groups. [8]
A meta-analysis published in 2013 found that it is statistically significantly less efficacious than other second-generation antipsychotics. [9]
Has a higher incidence of extrapyramidal side effects than the other atypical antipsychotics, but still less than that seen with typical antipsychotics. [1] [10] A trend was observed in a clinical trial comparing mosapramine with perospirone that favoured perospirone for producing less prominent extrapyramidal side effects than mosapramine although statistical significant was not reached. [6] It may produce less QT interval prolongation than zotepine, as in one patient who had previously been on zotepine switching to perospirone corrected their prolonged QT interval. [11] It also tended to produce less severe extrapyramidal side effects than haloperidol in a clinical trial comparing the two (although statistical significance was not reached). [5]
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse. [12] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite. [13] Other symptoms may include restlessness, increased sweating, and trouble sleeping. [13] Less commonly there may be a felling of the world spinning, numbness, or muscle pains. [13] Symptoms generally resolve after a short period of time. [13]
There is tentative evidence that discontinuation of antipsychotics can result in psychosis. [14] It may also result in reoccurrence of the condition that is being treated. [15] Rarely tardive dyskinesia can occur when the medication is stopped. [13]
Perospirone binds to the following receptors with very high affinity (as an antagonist unless otherwise specified): [9] [16] [17] [18] [19] [20]
And the following receptor with high affinity: [9]
And the following with moderate affinity: [9]
And with low affinity for the following receptor: [9]
Withdrawal of antipsychotic drugs after long-term therapy should always be gradual and closely monitored to avoid the risk of acute withdrawal syndromes or rapid relapse.